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更新于：2025-01-24
Icaritin
阿可拉定
更新于：2025-01-24
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2022-01-10), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (中国)、附条件批准 (中国) |
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关联
23
项与 阿可拉定 相关的临床试验ChiCTR2400094250
Study on the Efficacy and Safety of Icaritin in the Treatment of Unresectable Hepatocellular Carcinoma (HCC) with Child-Pugh B and C Liver Function
NCT06644937
Single-arm Clinical Trial of TACE in Combination With Acoradine as Adjuvant Therapy After Surgery in Patients With Hepatocellular Carcinoma at High Risk of Recurrence
NCT06285149
Prospective Single-arm, Single-center Exploratory Clinical Study on Efficacy and Safety of Interventional Therapy Combined With Icaritin in First-line Treatment of Middle and Advanced HCC in Child Grade B Patients
100 项与 阿可拉定 相关的临床结果
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100 项与 阿可拉定 相关的转化医学
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100 项与 阿可拉定 相关的专利（医药）
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350
项与 阿可拉定 相关的文献（医药）2025-04-01BIOMATERIALS
Pulmonary delivery of dual-targeted nanoparticles improves tumor accumulation and cancer cell targeting by restricting macrophage interception in orthotopic lung tumors
Article
作者: Liao, Yonghong ; Sun, Tingting ; Liao, Yong-Hong ; Ma, Siqi ; Wang, Chenao ; Wei, Jia-Xing ; Sun, Ting-Ting ; Ma, Si-Qi ; Ge, Di ; Wei, Jiaxing ; Li, Yunfei ; Chen, Xiaoyuan ; Li, Yun-Fei ; Wang, Chen-Ao
Despite the recognized potential of inhaled nanomedicines to enhance and sustain local drug concentrations for lung cancer treatment, the influence of macrophage uptake on targeted nanoparticle delivery to and within tumors remains unclear. Here, we developed three ligand-coated nanoparticles for pulmonary delivery in lung cancer therapy: phenylboronic acid-modified nanoparticles (PBA-NPs), PBA combined with folic acid (FA-PBA-NPs), and PBA with mannose (MAN-PBA-NPs). In vitro, MAN-PBA-NPs were preferentially internalized by macrophages, whereas FA-PBA-NPs exhibited superior uptake by cancer cells compared to macrophages. Following intratracheal instillation into mice with orthotopic Lewis lung carcinoma tumors, all three nanoparticles showed similar lung retention. However, MAN-PBA-NPs were more prone to interception by lung macrophages, which limited their accumulation in tumor tissues. In contrast, both PBA-NPs and FA-PBA-NPs achieved comparable high tumor accumulation (∼11.3% of the dose). Furthermore, FA-PBA-NPs were internalized by ∼30% of cancer cells, significantly more than the 10-18% seen with PBA-NPs or MAN-PBA-NPs. Additionally, FA-PBA-NPs loaded with icaritin effectively inhibited the Wnt/β-catenin pathway, resulting in superior anti-tumor efficacy through targeted cancer cell delivery. Overall, FA-PBA-NPs demonstrated advantageous competitive uptake kinetics by cancer cells compared to macrophages, enhancing tumor targeting and therapeutic outcomes.
2025-02-01JOURNAL OF CONTROLLED RELEASE
Iodine-131 radioembolization boosts the immune activation enhanced by icaritin/resiquimod in hepatocellular carcinoma
Article
作者: Zhang, Jianping ; He, Simin ; Li, Xinyi ; Xu, Mingzhen ; Lu, Xin ; Qian, Yuyi ; Song, Shaoli
Transarterial radioembolization (TARE) is a recommended locoregional strategy for intermediate hepatocellular carcinoma (HCC), whereas, the effect is insufficient to reverse the immunosuppression tumor microenvironment, and the overall benefits for patients remain to be improved. In this study, a multifunctional microsphere (MS) 131I-ICT/R848-MS is developed to propose an approach combined with TARE, icaritin (ICT) and immune modulator resiquimod (R848). ICT and iodine-131 (131I) radiation can induce immunogenic cell death, which, in combination with R848, will boost dendritic cell (DC) maturation. Decellularized liver model and SPECT/CT imaging revealed high specificity and long retention of microspheres. Radioactive distribution of 131I in tumor on 7 d following 131I-MS injection was over 7 times of that in normal liver tissue (4.26 ± 1.21 % ID/g vs 0.57 ± 0.23 % ID/g). 131I-ICT/R848-MS embolization brought significant immune activation, where the ratio of cytotoxic T lymphocytes to regulatory T cells in tumor sites upregulated from 1.75 ± 0.20 to 24.31 ± 1.79, and DC maturation in lymph nodes increased from 8.90 ± 1.51 % to 34.70 ± 3.12 %. Enhanced anti-tumor efficacy with no relapse was proved in rat orthotopic N1S1 HCC models. These results demonstrated the great potential of this multifunctional embolic agent to treat HCC through transarterial radio-immuno-chemoembolization (TARICE).
2025-01-15ACS Applied Materials & Interfaces
Mitochondria-Targeted Icaritin Nanoparticles Induce Immunogenic Cell Death in Hepatocellular Carcinoma
Article
作者: Xu, Xiao ; Hu, Haitao ; Sun, Yiyang ; Zhang, Zhouxing ; Zhang, Jing ; Qiu, Nasha ; Xu, Shengjun ; Liu, Yanpeng ; Shen, Youqing ; Xie, Yangla ; Xie, Chang ; Chen, Siyu
Hepatocellular carcinoma (HCC) is a highly malignant tumor that is resistant to chemotherapy and immunotherapy. Icaritin (ICT), a traditional Chinese medicine, has been reported as an immunoregulatory agent for treating advanced unresectable HCC. ICT induces mitophagy to cause immunogenic cell death (ICD); however, the poor bioavailability of ICT limits its therapeutic efficacy and clinical use. Therefore, this study aimed to assess the effect of using the poly(2-(N-oxide-N,N-diethylamino) ethyl methacrylate)-b-poly(ε-caprolactone) copolymer (OPDEA-PCL) to encapsulate ICT into nanoparticles (ICT NPs). OPDEA-PCL/ICT NPs colocalized with the mitochondria, promoting the ICD induction effect of ICT in mouse HCC H22 cells. In the H22 subcutaneous tumor model, intravenously injected OPDEA-PCL/ICT NPs quickly accumulated in the tumor and efficiently activated systemic anticancer immunogenicity through their effects on mitophagy. The resulting tumor suppression rate was 60%, which was significantly higher than that of free ICT and poly(ethylene glycol) (PEG)-PCL/ICT NPs. Furthermore, mouse survival was also prolonged by nearly 2-fold with OPDEA-PCL/ICT NPs compared with PBS. In summary, this approach provides valuable insights into improving the immunotherapeutic efficacy of ICT for HCC.
100 项与 阿可拉定 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 肝细胞癌 | 中国 | 2022-01-10 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 不可切除的肝细胞癌 | 临床3期 | 中国 | 2022-12-12 | |
| 肝癌 | 临床3期 | 中国 | 2022-01-30 | |
| 晚期肝细胞癌 | 临床3期 | 中国 | 2017-09-08 | |
| 乙型肝炎病毒相关肝细胞癌 | 临床3期 | 中国 | 2017-09-08 | |
| 晚期癌症 | 临床1期 | 中国 | 2011-11-28 | |
| 晚期恶性实体瘤 | 临床1期 | 中国 | 2011-11-01 | |
| 晚期乳腺癌 | 临床1期 | 中国 | 2010-11-01 | |
| 转移性乳腺癌 | 临床1期 | 中国 | 2010-11-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 283 | 壓壓鬱範鏇夢簾願窪構(觸觸製窪鏇夢艱構築選) = 糧廠鹽網夢夢鹽襯夢廠 遞窪鏇繭鑰衊夢製糧鹽 (繭遞夢夢夢鑰鑰積餘衊 ) 更多 | 积极 | 2021-05-20 | |||
huachashu | 壓壓鬱範鏇夢簾願窪構(觸觸製窪鏇夢艱構築選) = 簾構鹹願壓鏇壓鑰憲憲 遞窪鏇繭鑰衊夢製糧鹽 (繭遞夢夢夢鑰鑰積餘衊 ) 更多 | ||||||
临床1期 | 20 | 鬱築夢艱鏇鏇鏇構齋餘(襯膚遞鹹遞範壓鹽齋鹽) = 築鏇鏇鏇獵獵獵醖蓋簾 蓋衊襯選選糧簾鑰獵顧 (鏇蓋顧齋蓋鬱製廠醖網 ) 更多 | 积极 | 2019-03-28 | |||
N/A | - | - | 蓋積遞簾憲範製築獵簾(糧廠壓鑰襯鹹鹹艱網憲) = 窪鏇襯繭製襯遞願廠齋 鹽鹽窪願鹹獵鹽鏇醖鹽 (願蓋膚觸齋網艱簾鏇鹹 ) 更多 | 积极 | 2015-04-17 |
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